LY-178210-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

LY178210

Cat.No.:HY-129481

CASNo.:114943-19-0

分⼦式:C₁₈H₂₅N₃O

分⼦量:299.41

作⽤靶点:5-HTReceptor

作⽤通路:GPCR/GProtein;NeuronalSignaling

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性LY178210(Compound24)是⼀种选择性的5-羟⾊胺1A受体(5-HT1Areceptor)部分激动剂,其对5-HT1A

受体和5-HT1D受体的Ki分别为0.67和380nM。LY178210对α₂-肾上腺素能受体、5-HT₂等神经递质受体

⼏乎⽆活性。LY178210抑制Foscolin刺激的环化酶活性,但最⼤效能低于完全激动剂8-OH-DPAT(HY-

112061)。LY178210显著降低⼤下丘脑5-羟基吲哚⼄酸(5-HIAA)⽔平并提升了⾎清⽪质酮浓度。

IC50Target5-HT1AReceptor5-HT1DReceptor

0.67nM(IC50)380nM(IC50)

REFERENCES

[1].FlaughME,etal.6-substituted1,3,4,5-tetrahydrobenz[cd]indol-4-amines:potentserotoninagonists.JMedChem.1988Sep;31(9):1746-

53.

[2].SlaughterJL,etal.6-substitutedtricyclicpartialergolinecompoundsareselectiveandpotent5-hydroxytryptamine1Areceptoragents.

LifeSci.1990;47(15):1331-7

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